Mutation in an adaptor protein PDZK1 affects transport activity of organic cation transporter OCTNs and oligopeptide transporter PEPT2.

abstract：:Eight covalent tyrosine kinase inhibitors (TKIs) were investigated to determine the characteristics of their covalent binding to plasma proteins. The data revealed that their covalent binding to plasma proteins is of species difference. In addition to the reports on neratinib and pyrotinib, osimertinib, alflutinib, AS...

journal_title：Drug metabolism and pharmacokinetics

authors： Liu X,Feng D,Zheng M,Cui Y,Zhong D

更新日期：2020-10-01 00:00:00

abstract：:Maleic acid (MA) was purposefully adulterated in an array of starch-based foods in Taiwan, inciting a food safety incident. Due to limited data on the pharmacokinetics and bioavailability of ingested MA, we studied pharmacokinetic (PK) parameters in serum and urine of Sprague Dawley rats. Three groups of male and fema...

journal_title：Drug metabolism and pharmacokinetics

authors： Wu C,Chen HC,Luo YS,Chiang SY,Wu KY

更新日期：2016-12-01 00:00:00

abstract：:Human carboxylesterase 1 (hCE-1, CES1A1, HU1) and carboxylesterase 2 (hCE-2, hiCE, HU3) are a serine esterase involved in both drug metabolism and activation. Although both hCE-1 and hCE-2 are present in several organs, the hydrolase activity of liver and small intestine is predominantly attributed to hCE-1 and hCE-2,...

journal_title：Drug metabolism and pharmacokinetics

authors： Imai T

更新日期：2006-06-01 00:00:00

abstract：:Studies of the genetic regulation involved in drug metabolizing enzymes and drug transporters are of great interest to understand the molecular mechanisms of drug response and toxic events. Recent reports have revealed that hydrophobic ligands and several nuclear receptors are involved in the induction or down-regulat...

journal_title：Drug metabolism and pharmacokinetics

authors： Nakata K,Tanaka Y,Nakano T,Adachi T,Tanaka H,Kaminuma T,Ishikawa T

更新日期：2006-12-01 00:00:00

abstract：:Microdose (MD) clinical trials have been introduced to obtain human pharmacokinetic data early in drug development. Here we assessed the cost-effectiveness of microdose integrated drug development in a hypothetical model, as there was no such quantitative research that weighed the additional effectiveness against the ...

journal_title：Drug metabolism and pharmacokinetics

authors： Yamane N,Igarashi A,Kusama M,Maeda K,Ikeda T,Sugiyama Y

更新日期：2013-01-01 00:00:00

abstract：:Standard incubation procedures for carrying out microsomal assays involve the use of less than 1% w/v organic solvents to minimize the potential inhibitory effects of organic solvents on metabolic activity. This presents a practical limitation for poorly soluble xenobiotics, which cannot be incubated at concentrations...

journal_title：Drug metabolism and pharmacokinetics

authors： Argikar UA,Liang G,Bushee JL,Hosagrahara VP,Lee W

更新日期：2011-01-01 00:00:00

abstract：:Pitavastatin undergoes little hepatic metabolism but it is a substrate for uptake and efflux transporters, particularly OATP1B1 (gene SLCO1B1). A previous study in 8 Japanese healthy subjects showed that co-administration with grapefruit juice (GFJ) resulted in a small increase in systemic exposure to pitavastatin. We...

journal_title：Drug metabolism and pharmacokinetics

authors： Hu M,Mak VW,Yin OQ,Chu TT,Tomlinson B

更新日期：2013-01-01 00:00:00

abstract：:Tuftsin, a natural phagocytosis-stimulating tetrapeptide, had aroused much interest in tumor immunotherapy, but the poor pharmacokinetics hampered its clinical developments, for that it was extremely susceptible to degradation by enzymolysis in vivo. T Peptide (TP) was a newly designed tuftsin derivative aimed to enha...

journal_title：Drug metabolism and pharmacokinetics

authors： Gu R,He Y,Han S,Yuan S,An Y,Meng Z,Zhu X,Gan H,Wu Z,Li J,Zheng Y,Zhang L,Gao L,Dou G

更新日期：2016-02-01 00:00:00

abstract：:1. Assay methods to detect drug interaction in toxicological samples were established by determining cytochrome P450 content and its activity in liver samples. The O-dealkylation reaction of 7-alkoxycoumarin was indicated to reflect changes in the molecular forms of P450s, and the enzyme induction or inhibition in the...

journal_title：Drug metabolism and pharmacokinetics

authors： Matsubara T

更新日期：2002-01-01 00:00:00

abstract：:In vivo percutaneous absorption of emedastine difumarate was investigated in rats and compared with rat skin in vitro. Since emedastine entering the systemic circulation is mostly excreted in bile, we first came up with the method of collecting bile with a minimal skin incision. In vivo skin permeation of the drug was...

journal_title：Drug metabolism and pharmacokinetics

authors： Harada S,Yamashita F,Hashida M

更新日期：2005-10-01 00:00:00

abstract：:The object of this analysis was to develop a population pharmacokinetic model of micafungin, a new anti-fungal agent of the echinocandin class, to optimize dosing in Japanese patients with fungal infections. Population pharmacokinetics parameters were determined using NONMEM based on pharmacokinetic data from 198 subj...

journal_title：Drug metabolism and pharmacokinetics

authors： Tabata K,Katashima M,Kawamura A,Kaibara A,Tanigawara Y

更新日期：2006-08-01 00:00:00

abstract：:The ATP-binding cassette transporter, ABCG2, which is expressed at high levels in the intestine and liver, functions as an efflux transporter for many drugs, including clinically used anticancer agents such as topotecan and the active metabolite of irinotecan (SN-38). In this study, to elucidate the linkage disequilib...

journal_title：Drug metabolism and pharmacokinetics

authors： Maekawa K,Itoda M,Sai K,Saito Y,Kaniwa N,Shirao K,Hamaguchi T,Kunitoh H,Yamamoto N,Tamura T,Minami H,Kubota K,Ohtsu A,Yoshida T,Saijo N,Kamatani N,Ozawa S,Sawada J

更新日期：2006-04-01 00:00:00

abstract：:A novel method for the prediction of drug-drug interaction has been established based on the in vitro metabolic stability in the "serum incubation method" using cryopreserved human hepatocytes suspended in 100% human serum. As a novel approach, the inhibitory effect of inhibitors on the metabolism of substrates during...

journal_title：Drug metabolism and pharmacokinetics

authors： Shibata Y,Takahashi H,Chiba M,Ishii Y

更新日期：2008-01-01 00:00:00

abstract：UNLABELLED:Better prediction of drug disposition prior to the clinical trial is critical for the efficient development of new drugs. The purpose of this study is to develop a novel multiple assessment methodology of hepatocellular drug disposition from drug uptake to efflux including biliary and basolateral excretion, ...

journal_title：Drug metabolism and pharmacokinetics

authors： Takahashi R,Ichikawa H,Kanda K

更新日期：2016-04-01 00:00:00

abstract：:We studied the intrahepatic disposition characteristics of galactosylated polyethylenimine (Gal-PEI)/plasmid DNA (pDNA) complexes using rat liver perfusion experiment. After intraportal administration, transfection activity in liver of Gal-PEI complexes was approximately 26-fold higher than that of native PEI complexe...

journal_title：Drug metabolism and pharmacokinetics

authors： Fumoto S,Kawakami S,Ishizuka M,Nishikawa M,Yamashita F,Hashida M

更新日期：2003-01-01 00:00:00

abstract：:The present study was undertaken to characterize the transport of (3-methyl-His(2)) thyrotropin-releasing hormone ([(3)H]MeTRH) across the blood-brain barrier in mice and the effects of thyrotropin-releasing hormone (TRH) and its analogues (taltirelin and montirelin) on the transport and brain distribution. Integratio...

journal_title：Drug metabolism and pharmacokinetics

authors： Urayama A,Yamada S,Ohmori Y,Deguchi Y,Uchida S,Kimura R

更新日期：2003-01-01 00:00:00

abstract：:The concentration and distribution of a drug or its metabolites in tissues are key factors for understanding drug efficacy or toxicity. Conventional pharmacokinetic studies show that the plasma concentration of a drug is often unrelated to the intra-tissue concentration. Moreover, it is difficult to predict the distri...

journal_title：Drug metabolism and pharmacokinetics

authors： Nishidate M,Hayashi M,Aikawa H,Tanaka K,Nakada N,Miura SI,Ryu S,Higashi T,Ikarashi Y,Fujiwara Y,Hamada A

更新日期：2019-08-01 00:00:00

abstract：:Specific antibody production is an important issue in crossover pharmacokinetic (PK) studies of protein-based formulations. We recently reported that intravenous co-administration of tacrolimus with multiple human interferon-alpha (h-IFN) administrations successfully suppressed the production of anti-h-IFN antibodies ...

journal_title：Drug metabolism and pharmacokinetics

authors： Yamazaki H,Miyake M,Kamada N,Nishibayashi T,Mukai T,Odomi M,Ishida T,Kiwada H

更新日期：2010-01-01 00:00:00

abstract：:In a clinical setting, changes in pharmacokinetics due to drug-drug interactions can often directly affect the therapeutic safety and efficacy of drugs. Recently, interest has been shown in drug-drug interactions in the intestine. It is now recognized that changes in the functions of drug transporters substantially in...

journal_title：Drug metabolism and pharmacokinetics

authors： Segawa M,Ogura J,Seki S,Itagaki S,Takahashi N,Kobayashi M,Hirano T,Yamaguchi H,Iseki K

更新日期：2013-01-01 00:00:00

abstract：:It is now widely appreciated that drug metabolites, in addition to the parent drugs themselves, can mediate the serious adverse effects exhibited by some new therapeutic agents, and as a result, there has been heightened interest in the field of drug metabolism from researchers in academia, the pharmaceutical industry...

journal_title：Drug metabolism and pharmacokinetics

authors： Baillie TA,Rettie AE

更新日期：2011-01-01 00:00:00

abstract：:The injectable form of oxycodone contains hydrocotarnine that is supposed to potentiate the analgesic effect of oxycodone with unknown mechanism(s). In this study, the effects of hydrocotarnine on the cytochrome P450 (CYP) and P-glycoprotein (P-gp) were investigated. Hydrocotarnine did not induce a significant change ...

journal_title：Drug metabolism and pharmacokinetics

authors： Ito K,Kubota Y,Toda T,Suto S,Ikarashi N,Sugiyama K

更新日期：2009-01-01 00:00:00

abstract：:The objective of this work was to develop a population pharmacokinetic model to assess the influence of subject covariates on the pharmacokinetics of valsartan in children. Data were collected from a single dose study in 26 hypertensive children ages 1 to 16 years. Subjects received 2 mg/kg valsartan suspension up to ...

journal_title：Drug metabolism and pharmacokinetics

authors： Habtemariam B,Sallas W,Sunkara G,Kern S,Jarugula V,Pillai G

更新日期：2009-01-01 00:00:00

abstract：:The mRNA levels of human cytochrome P450 (CYP)2Cs and CYP3As in primary cultures of freshly isolated human hepatocytes were assessed after exposure to NO-1886 and rifampicin, a typical inducer of CYP3As. mRNA levels were analyzed by real-time RT-PCR using an ABI PRISM 7700 Sequence Detector system. Exposure to NO-1886...

journal_title：Drug metabolism and pharmacokinetics

authors： Morioka Y,Nishimura M,Imai T,Suzuki S,Harada M,Satoh T,Naito S

更新日期：2006-02-01 00:00:00

abstract：:Morphine is one of the strongest analgesics and is commonly used for the treatment of chronic pain. The pharmacokinetic properties of morphine are, in part, modulated by P-glycoprotein (P-gp). We previously reported that intestinal P-gp expression levels are influenced via the activation of inducible nitric oxide synt...

journal_title：Drug metabolism and pharmacokinetics

authors： Nawa A,Fujita-Hamabe W,Kishioka S,Tokuyama S

更新日期：2011-01-01 00:00:00

abstract：:Olopatadine, a new second-generation antihistamine, is widely used in the treatment of allergic disorders. The low levels of histamine H1 receptor occupancy in human brain by olopatadine, which is related to its minimal sedation, suggest its low penetration into the brain. The present study evaluates the impact of P-g...

journal_title：Drug metabolism and pharmacokinetics

authors： Mimura N,Nagata Y,Kuwabara T,Kubo N,Fuse E

更新日期：2008-01-01 00:00:00

abstract：:Dihydrofolate reductase gene (DHFR) 19-bp deletion polymorphisms result in varied DHFR enzymatic activity affecting the risk for preterm delivery, spina bifida, and the efficacy of methotrexate (MTX). Ethnic differences in DHFR 19-bp polymorphisms may be responsible for the divergent findings in previous genetic studi...

journal_title：Drug metabolism and pharmacokinetics

authors： Hayashi H,Horino M,Morishita M,Tazoe Y,Tsuboi S,Matsuyama T,Kosuge K,Yamada H,Tsuji D,Inoue K,Itoh K

更新日期：2010-01-01 00:00:00

abstract：:Decitabine (DAC), a DNA methylation inhibitor, is transported into cancer cells mainly via equilibrative nucleoside transporter 1 (ENT1) and subsequently phosphorylated by deoxycytidine kinase (dCK). We previously reported that apparent DAC uptake into cells may be described using a simple compartment model with clear...

journal_title：Drug metabolism and pharmacokinetics

authors： Ueda K,Nakamura T,Tanaka S,Hosokawa M,Iwakawa S,Ogawara KI

更新日期：2020-02-01 00:00:00

abstract：:Pept2 knockout mice are an important tool to evaluate the evolving role and relevance of this proton-coupled oligopeptide transporter beyond drug disposition, where the transporter also modulates the pharmacodynamic and toxicodynamic effects of drug substrates. Our in vivo studies with glycylsarcosine in Pept2 knockou...

journal_title：Drug metabolism and pharmacokinetics

authors： Kamal MA,Keep RF,Smith DE

更新日期：2008-01-01 00:00:00

abstract：:The participation of cytochrome P-450 (CYP) isoforms in the metabolism of selegiline was investigated. Experiments using recombinant CYP isoforms expressed in human lymphoblastoid cells showed CYP2B6 to be the major CYP isoform involved with the metabolism of selegiline. CYP1A2 and CYP3A4 also contributed to the metab...

journal_title：Drug metabolism and pharmacokinetics

authors： Kamada T,Chow T,Hiroi T,Imaoka S,Morimoto K,Ohde H,Funae Y

更新日期：2002-01-01 00:00:00

abstract：:The purpose of the present study was to evaluate and compare the absolute protein expression levels of 28 drug-related transporters in Caco-2 cell monolayers cultured for 2, 3, and 4 weeks. Plasma membrane fractions of Caco-2 cells cultured on Transwell inserts for 2, 3 and 4 weeks were prepared and digested with tryp...

journal_title：Drug metabolism and pharmacokinetics

authors： Uchida Y,Ohtsuki S,Kamiie J,Ohmine K,Iwase R,Terasaki T

更新日期：2015-04-01 00:00:00